JP2011520903A5 - - Google Patents
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- Publication number
- JP2011520903A5 JP2011520903A5 JP2011509679A JP2011509679A JP2011520903A5 JP 2011520903 A5 JP2011520903 A5 JP 2011520903A5 JP 2011509679 A JP2011509679 A JP 2011509679A JP 2011509679 A JP2011509679 A JP 2011509679A JP 2011520903 A5 JP2011520903 A5 JP 2011520903A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- salt
- cyano
- salt according
- cyclopenta
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 3
- 201000001881 impotence Diseases 0.000 claims 3
- 208000029725 Metabolic bone disease Diseases 0.000 claims 2
- 206010049088 Osteopenia Diseases 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- 210000000988 bone and bone Anatomy 0.000 claims 2
- 210000003205 muscle Anatomy 0.000 claims 2
- FBCDRHDULQYRTB-UHFFFAOYSA-N 2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-1h-imidazo[5,1-f][1,2,4]triazin-4-one;trihydrate;hydrochloride Chemical compound O.O.O.Cl.CCCC1=NC(C)=C(C(N=2)=O)N1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(CC)CC1 FBCDRHDULQYRTB-UHFFFAOYSA-N 0.000 claims 1
- KBRSJPHSCOAFDR-UHFFFAOYSA-N 3-chloro-6-methyl-5,5-dioxo-11h-benzo[c][2,1]benzothiazepin-11-ol Chemical compound O=S1(=O)N(C)C2=CC=CC=C2C(O)C2=CC=C(Cl)C=C21 KBRSJPHSCOAFDR-UHFFFAOYSA-N 0.000 claims 1
- -1 5-fluoro-2-hydroxy-benzyl Chemical group 0.000 claims 1
- PKKNBXJMCHCHSP-INIZCTEOSA-N C(N)(OC(C)(C)[C@H]1CC2=C(N(C=3C=CC(=CC23)C#N)CC2=C(C=CC=C2)O)C1)=O Chemical class C(N)(OC(C)(C)[C@H]1CC2=C(N(C=3C=CC(=CC23)C#N)CC2=C(C=CC=C2)O)C1)=O PKKNBXJMCHCHSP-INIZCTEOSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- RUXJDAYOICLRHH-INIZCTEOSA-N propan-2-yl n-[(2s)-7-cyano-4-[(3-fluoro-2-hydroxyphenyl)methyl]-2,3-dihydro-1h-cyclopenta[b]indol-2-yl]carbamate Chemical compound C([C@H](C1)NC(=O)OC(C)C)C2=C1C1=CC(C#N)=CC=C1N2CC1=CC=CC(F)=C1O RUXJDAYOICLRHH-INIZCTEOSA-N 0.000 claims 1
- GAVLUGRJEJKCRF-RVHYNSKXSA-N propan-2-yl n-[(2s)-7-cyano-4-[[(2r,3s)-3-hydroxy-1-methylpyrrolidin-2-yl]methyl]-2,3-dihydro-1h-cyclopenta[b]indol-2-yl]carbamate Chemical compound C([C@H](C1)NC(=O)OC(C)C)C2=C1C1=CC(C#N)=CC=C1N2C[C@@H]1[C@@H](O)CCN1C GAVLUGRJEJKCRF-RVHYNSKXSA-N 0.000 claims 1
- 229960002639 sildenafil citrate Drugs 0.000 claims 1
- DEIYFTQMQPDXOT-UHFFFAOYSA-N sildenafil citrate Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 DEIYFTQMQPDXOT-UHFFFAOYSA-N 0.000 claims 1
- 229960000835 tadalafil Drugs 0.000 claims 1
- IEHKWSGCTWLXFU-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C([C]4C=CC=CC4=N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 IEHKWSGCTWLXFU-IIBYNOLFSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 229960001540 vardenafil hydrochloride Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5372208P | 2008-05-16 | 2008-05-16 | |
| US61/053,722 | 2008-05-16 | ||
| PCT/US2009/043875 WO2009140448A1 (en) | 2008-05-16 | 2009-05-14 | Tetrahydrocyclopenta[b]indole androgen receptor modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011520903A JP2011520903A (ja) | 2011-07-21 |
| JP2011520903A5 true JP2011520903A5 (OSRAM) | 2012-06-28 |
| JP5603327B2 JP5603327B2 (ja) | 2014-10-08 |
Family
ID=40847864
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011509679A Active JP5603327B2 (ja) | 2008-05-16 | 2009-05-14 | テトラヒドロシクロペンタ[b]インドールアンドロゲン受容体調節物質 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8486943B2 (OSRAM) |
| EP (1) | EP2297100B1 (OSRAM) |
| JP (1) | JP5603327B2 (OSRAM) |
| KR (1) | KR101278788B1 (OSRAM) |
| CN (1) | CN102026974B (OSRAM) |
| AU (1) | AU2009246348B2 (OSRAM) |
| BR (1) | BRPI0912394A2 (OSRAM) |
| CA (1) | CA2724629C (OSRAM) |
| CY (1) | CY1113341T1 (OSRAM) |
| DK (1) | DK2297100T3 (OSRAM) |
| EA (1) | EA019713B1 (OSRAM) |
| ES (1) | ES2396612T3 (OSRAM) |
| HR (1) | HRP20120917T1 (OSRAM) |
| MX (1) | MX2010012436A (OSRAM) |
| PL (1) | PL2297100T3 (OSRAM) |
| PT (1) | PT2297100E (OSRAM) |
| SI (1) | SI2297100T1 (OSRAM) |
| WO (1) | WO2009140448A1 (OSRAM) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA98777C2 (en) | 2006-11-20 | 2012-06-25 | Эли Лилли Энд Компани | Tetrahydrocyclopenta[b]indole compounds as androgen receptor modulators |
| US8268872B2 (en) | 2008-02-22 | 2012-09-18 | Radius Health, Inc. | Selective androgen receptor modulators |
| BRPI0907844B8 (pt) | 2008-02-22 | 2021-05-25 | Radius Health Inc | compostos e método para modular um receptor de andrógeno, processos de preparação e composição farmacêutica dos mesmos e seus usos |
| US8987319B2 (en) | 2010-02-04 | 2015-03-24 | Radius Health, Inc. | Selective androgen receptor modulators |
| PT2568806T (pt) | 2010-05-12 | 2016-08-05 | Radius Health Inc | Regimes terapêuticos |
| US8642632B2 (en) | 2010-07-02 | 2014-02-04 | Radius Health, Inc. | Selective androgen receptor modulators |
| WO2012047617A1 (en) | 2010-09-28 | 2012-04-12 | Radius Health, Inc. | Selective androgen receptor modulators |
| US9421264B2 (en) | 2014-03-28 | 2016-08-23 | Duke University | Method of treating cancer using selective estrogen receptor modulators |
| PL3122426T3 (pl) | 2014-03-28 | 2023-05-15 | Duke University | Leczenie raka sutka z zastosowaniem selektywnych modulatorów receptora estrogenowego |
| JOP20180072A1 (ar) * | 2014-09-11 | 2019-01-30 | Lilly Co Eli | علاج الأعراض المرتبطة بالعلاج بالحرمان من الأندروجين |
| SMT202200199T1 (it) | 2016-06-22 | 2022-07-21 | Ellipses Pharma Ltd | Metodi di trattamento del cancro del seno ar+. |
| US20180185347A1 (en) * | 2016-11-16 | 2018-07-05 | Transition Therapeutics (Ireland 2) Limited | Tetrahydrocyclopenta[b]indole compounds and phosphodiesterase inhibitors for the treatment of the signs and symptoms of bhp |
| EP4374925A3 (en) | 2017-01-05 | 2025-01-15 | Radius Pharmaceuticals, Inc. | Polymorphic forms of rad1901-2hcl |
| CN112423844B (zh) | 2018-07-04 | 2024-08-13 | 雷迪厄斯制药公司 | Rad1901-2hcl的多晶型形式 |
| CN119390714A (zh) | 2019-02-12 | 2025-02-07 | 雷迪厄斯制药公司 | 方法和化合物 |
| EP4096660A1 (en) * | 2020-01-27 | 2022-12-07 | EirGen Pharma Ltd. | Tetrahydrocyclopenta[b]indole compounds for the treatment of renal disease |
| EP4175647A4 (en) * | 2020-07-06 | 2024-08-07 | Crescenta Biosciences | ANTIVIRAL USE OF COMPOUNDS MODULATING FABP4 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4988820A (en) | 1986-02-21 | 1991-01-29 | Bayer Aktiengesellschaft | Cycloalkano(1,2-B) indole-sulponamides |
| GB8924392D0 (en) | 1989-10-30 | 1989-12-20 | Bayer Ag | Substituted cycloalkano/b/dihydroindole-and-indolesulphonamides |
| GB9008108D0 (en) | 1990-04-10 | 1990-06-06 | Bayer Ag | Cycloalkano(b)dihydroindoles and-indolesulphonamides substituted by heterocycles |
| DE4027278A1 (de) | 1990-08-29 | 1992-03-05 | Bayer Ag | Heterocyclisch substituierte indolsulfonamide |
| DE4131346A1 (de) | 1991-09-20 | 1993-03-25 | Bayer Ag | Indolsulfonamid substituierte dihydropyridine, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln |
| US7160909B2 (en) | 2001-08-09 | 2007-01-09 | Eli Lilly And Company | Cyclopenta[b]indole derivatives as sPLA2 inhibitors |
| DE10164564B4 (de) | 2001-12-14 | 2007-05-16 | Zentaris Gmbh | Tetrahydrocarbazolderivate als Liganden für G-Protein gekoppelte Rezeptoren (GPCR) |
| US7534897B2 (en) | 2002-05-16 | 2009-05-19 | Shionogi & Co., Ltd. | Indole arylsulfonaimide compounds exhibiting PGD 2 receptor antagonism |
| US20060074124A1 (en) | 2003-09-12 | 2006-04-06 | Andrew Napper | Methods of treating a disorder |
| US7019022B2 (en) | 2003-12-15 | 2006-03-28 | Merck Frosst Canada & Co. | Substituted tetrahydrocarbazole and cyclopentanoindole derivatives |
| EP1723105B1 (en) | 2004-03-03 | 2013-05-15 | Eli Lilly And Company | Bicyclic substituted indole-derivative steroid hormone nuclear receptor modulators |
| JP2008520742A (ja) | 2004-11-23 | 2008-06-19 | ピーティーシー セラピューティクス, インコーポレイテッド | Vegf産生の阻害に有用なカルバゾール誘導体、カルボリン誘導体およびインドール誘導体 |
| EP1856126A2 (en) * | 2005-02-17 | 2007-11-21 | Wyeth a Corporation of the State of Delaware | Cycloalkylfused indole, benzothiophene, benzofuran and indene derivatives |
| JP5204650B2 (ja) | 2005-06-24 | 2013-06-05 | イーライ リリー アンド カンパニー | アンドロゲン受容体調節物質として有用なテトラヒドロカルバゾール誘導体 |
| US20090022694A1 (en) | 2005-10-18 | 2009-01-22 | Distefano Peter | Sirt1 inhibition |
| WO2008019825A1 (en) | 2006-08-14 | 2008-02-21 | Santhera Pharmaceuticals (Schweiz) Ag | Use of tricyclic indole derivatives for the treatment of muscular diseases |
| UA98777C2 (en) * | 2006-11-20 | 2012-06-25 | Эли Лилли Энд Компани | Tetrahydrocyclopenta[b]indole compounds as androgen receptor modulators |
-
2009
- 2009-05-14 EP EP09747531A patent/EP2297100B1/en active Active
- 2009-05-14 DK DK09747531.3T patent/DK2297100T3/da active
- 2009-05-14 US US12/989,959 patent/US8486943B2/en active Active
- 2009-05-14 PT PT97475313T patent/PT2297100E/pt unknown
- 2009-05-14 AU AU2009246348A patent/AU2009246348B2/en not_active Ceased
- 2009-05-14 CA CA2724629A patent/CA2724629C/en not_active Expired - Fee Related
- 2009-05-14 CN CN200980117076XA patent/CN102026974B/zh active Active
- 2009-05-14 HR HRP20120917AT patent/HRP20120917T1/hr unknown
- 2009-05-14 SI SI200930447T patent/SI2297100T1/sl unknown
- 2009-05-14 MX MX2010012436A patent/MX2010012436A/es active IP Right Grant
- 2009-05-14 BR BRPI0912394A patent/BRPI0912394A2/pt not_active IP Right Cessation
- 2009-05-14 PL PL09747531T patent/PL2297100T3/pl unknown
- 2009-05-14 KR KR1020107025588A patent/KR101278788B1/ko not_active Expired - Fee Related
- 2009-05-14 WO PCT/US2009/043875 patent/WO2009140448A1/en not_active Ceased
- 2009-05-14 JP JP2011509679A patent/JP5603327B2/ja active Active
- 2009-05-14 ES ES09747531T patent/ES2396612T3/es active Active
- 2009-05-14 EA EA201071317A patent/EA019713B1/ru not_active IP Right Cessation
-
2012
- 2012-11-14 CY CY20121101095T patent/CY1113341T1/el unknown
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